P450
Cytochrome P450 are a family of heme-containing monoxygenases catalyzing the metabolism of xenobiotics in the body where P450 enzymes use O2 and two electrons provided by NAD(P)H with the help of redox partner flavoproteins and iron-sulfur proteins to catalyze the monooxygenation of a variety of substrates. Based on how electrons from NAD(P)H are delivered to the catalytic site, P450 enzymes are divided into four classes, including Class I requiring both an FAD-containing reductase and an iron sulfur redoxin, Class II requiring only an FAD/FMN-containg P450 reductase, Class III requiring no electron donor and Class IV requiring electrons directly from NAD(P)H.
- Cat.No. 产品名称 Information
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GC67933
LKY-047
LKY-047,是 Decursin 的一种衍生物,是一种有效的选择性的可逆竞争性的细胞色素 P45022J2 (CYP2J2) 抑制剂,IC50 为 1.7 μM。LKY-047 对其他人类 P450 无效,例如 CYP1A2、CYP2A6、CYP2B6、CYP2C8、CYP2C9、CYP2C19、CYP2D6、CYP2E1 和 CYP3A。
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GC66197
α-?Terpinyl acetate
α-Terpinyl acetate 是从 Laurus nobilis L. 精油中分离出的一种单萜酯。α-Terpinyl acetate 是竞争性的 P450 2B6 底物,与其活性部位结合的 Kd 值为 5.4 ?μM 。
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GC52132
N-desmethyl Diltiazem (hydrochloride)
An active metabolite of diltiazem
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GC65517
4-(Trifluoromethyl)umbelliferone
4-(Trifluoromethyl)umbelliferone 是大鼠肝细胞色素 P450 酶的荧光探针底物。
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GC65345
BI 653048
BI 653048 是一种选择性且口服的非甾体类糖皮质激素 (glucocorticoid (GC)) 激动剂,其 IC50 值为 55 nM。BI 653048 抑制 CP1A2,CYP2D6,CYP2C9,CYP2C19 和 CYP3A4 的活性并降低对 hERG 离子通道的亲和力 (IC50>30 μM)。BI 653048 源于专利 WO2005028501A1 (化合物 103),它也是一种 HCV NS3 protease 抑制剂,可以减少感染丙型肝炎病毒的病毒载量。
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GC65260
EDP-305
EDP-305 是一种口服有效且选择性的 farnesoid X 受体 (FXR) 激动剂,其 EC50 值为 34 nM (CHO 细胞嵌合性 FXR) 和 8 nM (HEK 细胞全长 FXR)。EDP-305 显示出强大而持久的抗纤维化作用。EDP-305 可用于原发性胆道胆管炎 (PBC) 和非酒精性脂肪性肝炎 (NASH) 研究。
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GC65088
Atovaquone-d5
Atovaquone-d5 (Atavaquone-d5) 是 Atovaquone 的氘代物。Atovaquone (Atavaquone) 是一种有效的、具有口服活性的选择性寄生虫线粒体细胞色素 bc1 (parasite's mitochondrial cytochrome bc1) 复合物的抑制剂。Atovaquone 抑制人类和 P. falciparum 细胞色素 bc1 活性,IC50 值分别为 460 nM 和 2.0 nM。Atovaquone 是一种抗疟 (antimalarial agent) 试剂,有潜力用于肺孢子虫肺炎、弓形体病、疟疾和巴贝斯虫病的相关研究。
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GC52083
21-Deoxycortisone
A corticosteroid metabolite of 11-keto progesterone
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GC52062
7-Benzyloxy-4-(trifluoromethyl)coumarin
A fluorogenic substrate for CYP1A2 and CYP3A
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GC52060
Trimipramine N-oxide
Trimipramine N-oxide 是三环抗抑郁药 trimipramine 的活性代谢物。
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GC52045
N-desmethyl Azelastine
N-去甲基氮卓斯汀是氮卓斯汀的主要活性代谢物,经细胞色素P450酶系统氧化代谢,蛋白结合率为97%,消除半衰期为54小时。
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GC52038
Desthiazolylmethyl Ritonavir
A ritonavir degradation product
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GC52024
Aripiprazole N-oxide
A metabolite of aripiprazole
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GC52019
Norpropranolol (hydrochloride)
An active metabolite of propranolol
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GC52007
N-hydroxylamine Dapsone
An active metabolite of dapsone
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GC49875
(±)-N-desmethyl Venlafaxine (hydrochloride)
A minor active metabolite of venlafaxine
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GC49866
Desmethyl Carvedilol
An active metabolite of carvedilol
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GC49855
Harmalol (hydrochloride hydrate)
A β-carboline alkaloid and an active metabolite of harmaline
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GC49851
Norquetiapine
An active metabolite of quetiapine
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GC49842
Digoxigenin Bisdigitoxoside
A Na+/K+-ATPase inhibitor
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GC49832
Hydroxymetronidazole
羟基甲硝唑 (Metronidazole-OH) 是甲硝唑的代谢物,属于硝基咪唑类。
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GC49817
Desethoxy Quetiapine (hydrochloride)
An active metabolite of quetiapine
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GC64010
Abiraterone decanoate
Abiraterone decanoate 是一种有效的 Abiraterone 前药。Abiraterone decanoate 通过肌肉内 (IM) 递送提供 Abiraterone 的受控释放和长效 CYP17 抑制。
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GC63872
Dagrocorat hydrochloride
Dagrocorat (PF-00251802) hydrochloride 是一种具有口服活性,选择性和高亲和性部分糖皮质激素受体的激动剂。Dagrocorat hydrochloride 也是一种时间依赖性可逆抑制剂,对 CYP3A (IC50=1.3 μM) 和CYP2D6 (Ki=0.57 μM) 有抑制作用。Dagrocorat hydrochloride 可用于类风湿性关节炎的研究。
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GC49686
N-desmethyl Regorafenib N-oxide
An active metabolite of regorafenib
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GC49629
6β-hydroxy Prednisolone
A metabolite of prednisolone
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GC49627
Rabeprazole sulfone
A metabolite of rabeprazole
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GC49583
N-desmethyl Sertraline (hydrochloride)
A metabolite of sertraline
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GC49559
Hydroxymethyl Tolperisone (hydrochloride)
A metabolite of tolperisone
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GC49544
8-hydroxy Mirtazapine
A metabolite of mirtazapine
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GC49503
Thujopsene
A sesquiterpene with diverse biological activities
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GC49501
Nirvanol
An active metabolite of mephenytoin
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GC63469
Abiraterone-D4
Abiraterone-D4 (CB-7598-D4) 是 Abiraterone 的氘代物。Abiraterone 是一种有效的不可逆的 CYP17A1 抑制剂,具有抗雄激素活性,抑制细胞色素 p450 酶 CYP17 的 17α-羟化酶和 17,20-裂合酶活性,IC50 值 分别为 2.5 nM 和 15 nM.
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GC63272
β-Apo-8’-carotenal
β-Apo-8’-carotenal (Apocarotenal) 是一种维生素原 A 类胡萝卜素,是大鼠CYP1A1 和 CYP1A2 的诱导剂。 β-Apo-8’-carotenal 存在于许多水果和蔬菜中。
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GC63199
Soticlestat
A cholesterol 24-hydroxylase/CYP46A1 inhibitor
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GC49439
(±)11(12)-DiHET MaxSpec® Standard
A quantitative analytical standard guaranteed to meet MaxSpec® identity, purity, stability, and concentration specifications
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GC49429
6-keto Lithocholic Acid
石胆酸的代谢产物
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GC49421
Atorvastatin lactone-d5
An internal standard for the quantification of atorvastatin lactone
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GC49410
CVT-2738
An active metabolite of ranolazine
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GC49409
Desmethyl Ranolazine
A metabolite of ranolazine
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GC49403
Benzarone
Benzarone (Fragivix) 是一种有效的人类尿酸转运蛋白 1 (hURAT1) 抑制剂,在卵母细胞中的 IC50 为 2.8 μM。
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GC49399
N-Desbutyl Dronedarone (hydrochloride)
决奈达隆的主要代谢物 Debutyldronedarone (SR35021) hydrochloride 是一种选择性甲状腺激素受体 α1 (TRα1) 抑制剂。
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GC49362
2-Amino-3,8-dimethylimidazo-[4,5-f]-quinoxaline
A food-derived carcinogen
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GC49355
Norfluoxetine-d5 (hydrochloride)
An internal standard for the quantification of norfluoxetine
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GC49320
7-Ethoxy-4-(trifluoromethyl)coumarin
7-Ethoxy-4-(trifluoromethyl)coumarin 是细胞色素 P450 超家族各种酶的荧光底物
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GC49291
rac-N-desmethyl Ivabradine-d6 (hydrochloride)
An internal standard for the quantification of N-desmethyl ivabradine
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GC49288
Dolutegravir M1
A metabolite of dolutegravir
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GC49281
SPA70
SPA70 是一种有效的选择性人孕烷 X 受体 (hPXR) 拮抗剂,IC50 为 540 nM (Ki=390 nM)。 SPA70可以增强癌细胞的化学敏感性。
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GC49230
Ferroprotoporphyrin
Ferroprotoporphyrin 是亚铁和卟啉的复合物,是脂肪酸与大鼠肝脏脂肪酸结合蛋白结合的等排抑制剂。
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GC49212
trans-carboxy Glimepiride
A metabolite of glimepiride